公开(公告)号：US11649255B2

公开(公告)日：2023-05-16

申请号：US17485711

申请日：2021-09-27

Applicant: 1st Biotherapeutics, Inc.

Inventor： Jinhwa Lee ,  Suyeon Jo ,  Keonseung Lim ,  A Yeong Park ,  Gadhe Changdev Gorakshnath ,  Hwajung Nam ,  Yeonguk Jeon ,  Yejin Hwang ,  Jae Eun Kim ,  Misoon Kim ,  Seung Mook Lim

IPC: C07F7/08 ,  C07D487/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04 ,  C07F9/6558

CPC classification number: C07F7/0812 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  C07F9/65583 ,  C07B2200/05

Abstract: The present disclosure provides a compound of Formula (I) or pharmaceutically acceptable salts thereof, a composition comprising the compound, methods of using the compound for the treatment of various disorders associated with HPK1, and methods of preparing these compounds.

公开(公告)号：US11649224B2

公开(公告)日：2023-05-16

申请号：US17313688

申请日：2021-05-06

Applicant: Cornell University

Inventor： Joseph P. Vacca ,  Dansu Li ,  Sarah Bettigole

IPC: C07D401/04 ,  C07D403/04 ,  A61P35/00 ,  C07D239/84 ,  C07D413/04 ,  C07D217/22 ,  C07D401/12 ,  C07D417/04 ,  A61K31/517

CPC classification number: C07D403/04 ,  A61K31/517 ,  A61P35/00 ,  C07D217/22 ,  C07D239/84 ,  C07D401/04 ,  C07D401/12 ,  C07D413/04 ,  C07D417/04

Abstract: Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.

公开(公告)号：US20230144106A1

公开(公告)日：2023-05-11

申请号：US17864133

申请日：2022-07-13

Applicant: Syros Pharmaceuticals, Inc.

Inventor： Jason J. Marineau ,  Peter B. Rahl ,  Kevin Sprott ,  Stephane Ciblat ,  Boubacar Sow ,  Robin Larouche-Gauthier ,  Lauren Berstler ,  Christopher Roberts ,  Yi Zhang ,  Francis Beaumier ,  Luce Lépissier

IPC: C07D417/04 ,  C07D417/14 ,  C07D495/04 ,  C07D513/02 ,  A61P35/00

CPC classification number: C07D417/04 ,  C07D417/14 ,  C07D495/04 ,  C07D513/02 ,  A61P35/00

Abstract: The present invention provides novel compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases, e.g., cancers (e.g., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angiogenesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject.

公开(公告)号：US11639352B2

公开(公告)日：2023-05-02

申请号：US17273659

申请日：2018-09-04

Applicant: Hoffmann-La Roche Inc.

Inventor： Wei Zhu ,  Ge Zou ,  Fabian Dey

IPC: C07D413/14 ,  A61K31/5377 ,  C07D417/14 ,  C07D417/04 ,  C07D471/08 ,  C07D471/10

Abstract: The present invention relates to compounds of formula (I), (I), wherein R1, R2 and R3 are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

公开(公告)号：US20230125481A1

公开(公告)日：2023-04-27

申请号：US17759490

申请日：2021-01-26

Applicant: EVOTEC INTERNATIONAL GMBH

Inventor： Christopher John BROWN ,  James Lindsay CARR ,  Mohamad SABBAH ,  Jeffrey Michael SCHKERYANTZ ,  Daryl Simon WALTER

IPC: C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D513/04 ,  C07D401/04

Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates, tautomers or stereoisomers thereof, wherein R1, R2, R2a, R3, Ra1, Ra2, Ra4, Ra5, X1, X1a, A1 and A2 have the meaning as indicated in the description and claims. The invention further relates to pharmaceutical compositions comprising said compounds, their use as medicament and in a method for treating and preventing of one or more diseases or disorders associated with integrated stress response.

公开(公告)号：US20230124361A1

公开(公告)日：2023-04-20

申请号：US17798552

申请日：2021-02-12

Applicant: CURADEV PHARMA PVT. LTD.

Inventor： Monali BANERJEE ,  Sourav BASU ,  Ritesh Kumar SHRIVASTAVA ,  David Cameron PRYDE ,  Sandip Kumar MIDDYA ,  Rajib GHOSH ,  Dharmendra B. YADAV ,  Arjun SURYA

IPC: C07D417/12 ,  C07D279/16 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D413/12 ,  C07D265/36 ,  C07D413/14 ,  C07D403/12 ,  C07D239/80 ,  C07D417/04

Abstract: The present invention relates to compounds of formula (I). The compounds maybe used to antagonise the Stimulator of Interferon Genes (STING) protein and may thereby treat liver fibrosis, fatty liver disease, non-alcoholic steatohepatitis (NASH), pulmonary fibrosis, lupus, sepsis, rheumatoid arthritis (RA), type I diabetes, STING-associated vasculopathy with onset in infancy (SAVI), Aicardi-Goutieres syndrome (AGS), familial chilblain lupus (FCL), systemic lupus erythematosus (SLE), retinal vasculopathy, neuroinflammation, systemic inflammatory response syndrome, pancreatitis, cardiovascular disease, renal fibrosis, stroke and age-related macular degeneration (AMD).

公开(公告)号：US20230123591A1

公开(公告)日：2023-04-20

申请号：US17962305

申请日：2022-10-07

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Marina Gelman ,  Todd Kinsella ,  Somasekhar Bhamidipati ,  Ihab Darwish ,  Rajinder Singh ,  Jiaxin Yu

IPC: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D471/04 ,  C07D519/00

Abstract: Disclosed are pyrazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein A, X, Z, m, p, and R2 are as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-β superfamily, and can be used to treat disease by blocking such activity.

公开(公告)号：US20230121195A1

公开(公告)日：2023-04-20

申请号：US17819602

申请日：2022-08-12

Applicant: Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft ,  Deutsches Krebsforschungszentrum

Inventor： Ilona GUTCHER ,  Ulrike RÖHN ,  Norbert SCHMEES ,  Ludwig ZORN ,  Lars RÖSE ,  Benjamin BADER ,  Christina KOBER ,  Rafael CARRETERO ,  Detlef STÖCKIGT ,  Horst IRLBACHER ,  Michael PLATTEN

IPC: C07D417/04 ,  A61P35/00 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D409/14 ,  C07D401/14

Abstract: The present invention covers 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compounds of general formula (1): in which X, R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.

公开(公告)号：US20230117418A1

公开(公告)日：2023-04-20

申请号：US17937210

申请日：2022-09-30

Applicant: Promega Corporation

Inventor： Matthew A. Larsen ,  Hui Wang ,  Wenhui Zhou ,  Peter Hofsteen ,  Jolanta Vidugiriene

IPC: C07D417/04 ,  C07D277/64

Abstract: Disclosed herein are compounds that can be used to selectively detect nitric oxide in samples. Also disclosed herein are compositions comprising the compounds and methods of detecting nitric oxide using the compounds.

公开(公告)号：US11629140B2

公开(公告)日：2023-04-18

申请号：US16532515

申请日：2019-08-06

Applicant: Feng-Wen Yen ,  Li-Chieh Chuang

Inventor： Feng-Wen Yen ,  Li-Chieh Chuang

IPC: C07D413/04 ,  C07D417/04 ,  C07D265/38 ,  C07F7/08 ,  C07D279/36 ,  C07D401/04 ,  H01L51/00

Abstract: An organic compound is described. An organic electroluminescence device comprises the organic compound, as a host of an emissive layer, or as a hole blocking layer. The organic compound may increase a half-life or current efficiency of the organic electroluminescence device. The organic compound may lower a driving voltage of the organic electroluminescence device. The mentioned organic compound may have the following formula: The same definition as described in the present invention.